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Items: 35

1.

Site-Specific Conjugation of the Indolinobenzodiazepine DGN549 to Antibodies Affords Antibody-Drug Conjugates with an Improved Therapeutic Index as Compared with Lysine Conjugation.

Bai C, Reid EE, Wilhelm A, Shizuka M, Maloney EK, Laleau R, Harvey L, Archer KE, Vitharana D, Adams S, Kovtun Y, Miller ML, Chari R, Keating TA, Yoder NC.

Bioconjug Chem. 2019 Dec 10. doi: 10.1021/acs.bioconjchem.9b00777. [Epub ahead of print]

PMID:
31747250
2.

Antibody-Drug Conjugates with Indolinobenzodiazepine Dimer Payloads: DNA-Binding Mechanism of Indolinobenzodiazepine Dimer Catabolites in Target Cancer Cells.

Singh R, Reid EE, Harris L, Salomon PL, Miller ML, Chari RVJ, Keating TA.

Mol Pharm. 2019 Dec 3. doi: 10.1021/acs.molpharmaceut.9b00675. [Epub ahead of print]

PMID:
31742408
3.

Synthesis and Evaluation of Camptothecin Antibody-Drug Conjugates.

Li W, Veale KH, Qiu Q, Sinkevicius KW, Maloney EK, Costoplus JA, Lau J, Evans HL, Setiady Y, Ab O, Abbott SM, Lee J, Wisitpitthaya S, Skaletskaya A, Wang L, Keating TA, Chari RVJ, Widdison WC.

ACS Med Chem Lett. 2019 Sep 6;10(10):1386-1392. doi: 10.1021/acsmedchemlett.9b00301. eCollection 2019 Oct 10.

4.

Optimizing Lysosomal Activation of Antibody-Drug Conjugates (ADCs) by Incorporation of Novel Cleavable Dipeptide Linkers.

Salomon PL, Reid EE, Archer KE, Harris L, Maloney EK, Wilhelm AJ, Miller ML, Chari RVJ, Keating TA, Singh R.

Mol Pharm. 2019 Oct 29. doi: 10.1021/acs.molpharmaceut.9b00696. [Epub ahead of print]

PMID:
31609629
5.

Synthesis of Highly Potent N-10 Amino-Linked DNA-Alkylating Indolinobenzodiazepine Antibody-Drug Conjugates (ADCs).

Archer KE, Reid EE, Shizuka M, Woods J, Harris L, Maloney EK, Bartle LM, Ab O, Wilhelm A, Setiady Y, Ponte JF, Singh R, Keating TA, Chari RVJ, Miller ML.

ACS Med Chem Lett. 2019 Jul 22;10(8):1211-1215. doi: 10.1021/acsmedchemlett.9b00254. eCollection 2019 Aug 8.

PMID:
31413807
6.

A Case Study Comparing Heterogeneous Lysine- and Site-Specific Cysteine-Conjugated Maytansinoid Antibody-Drug Conjugates (ADCs) Illustrates the Benefits of Lysine Conjugation.

Yoder NC, Bai C, Tavares D, Widdison WC, Whiteman KR, Wilhelm A, Wilhelm SD, McShea MA, Maloney EK, Ab O, Wang L, Jin S, Erickson HK, Keating TA, Lambert JM.

Mol Pharm. 2019 Sep 3;16(9):3926-3937. doi: 10.1021/acs.molpharmaceut.9b00529. Epub 2019 Jul 31.

PMID:
31287952
7.

A DNA-Interacting Payload Designed to Eliminate Cross-Linking Improves the Therapeutic Index of Antibody-Drug Conjugates (ADCs).

Miller ML, Shizuka M, Wilhelm A, Salomon P, Reid EE, Lanieri L, Sikka S, Maloney EK, Harvey L, Qiu Q, Archer KE, Bai C, Vitharana D, Harris L, Singh R, Ponte JF, Yoder NC, Kovtun Y, Lai KC, Ab O, Pinkas J, Keating TA, Chari RVJ.

Mol Cancer Ther. 2018 Mar;17(3):650-660. doi: 10.1158/1535-7163.MCT-17-0940. Epub 2018 Feb 13.

8.

Effects of Drug-Antibody Ratio on Pharmacokinetics, Biodistribution, Efficacy, and Tolerability of Antibody-Maytansinoid Conjugates.

Sun X, Ponte JF, Yoder NC, Laleau R, Coccia J, Lanieri L, Qiu Q, Wu R, Hong E, Bogalhas M, Wang L, Dong L, Setiady Y, Maloney EK, Ab O, Zhang X, Pinkas J, Keating TA, Chari R, Erickson HK, Lambert JM.

Bioconjug Chem. 2017 May 17;28(5):1371-1381. doi: 10.1021/acs.bioconjchem.7b00062. Epub 2017 Apr 13.

PMID:
28388844
9.

Understanding How the Stability of the Thiol-Maleimide Linkage Impacts the Pharmacokinetics of Lysine-Linked Antibody-Maytansinoid Conjugates.

Ponte JF, Sun X, Yoder NC, Fishkin N, Laleau R, Coccia J, Lanieri L, Bogalhas M, Wang L, Wilhelm S, Widdison W, Pinkas J, Keating TA, Chari R, Erickson HK, Lambert JM.

Bioconjug Chem. 2016 Jul 20;27(7):1588-98. doi: 10.1021/acs.bioconjchem.6b00117. Epub 2016 Jun 20.

PMID:
27174129
10.

Role of the Outer Membrane and Porins in Susceptibility of β-Lactamase-Producing Enterobacteriaceae to Ceftazidime-Avibactam.

Pagès JM, Peslier S, Keating TA, Lavigne JP, Nichols WW.

Antimicrob Agents Chemother. 2015 Dec 14;60(3):1349-59. doi: 10.1128/AAC.01585-15.

11.

In vitro activity of ceftazidime-avibactam against 338 molecularly characterized gentamicin-nonsusceptible Gram-negative clinical isolates obtained from patients in Canadian hospitals.

Denisuik AJ, Karlowsky JA, Denisuik T, Nichols WW, Keating TA, Adam HJ, Baxter M, Walkty A, Zhanel GG.

Antimicrob Agents Chemother. 2015;59(6):3623-6. doi: 10.1128/AAC.00364-15. Epub 2015 Mar 30.

12.

Activity of ceftazidime-avibactam against fluoroquinolone-resistant Enterobacteriaceae and Pseudomonas aeruginosa.

Pitart C, Marco F, Keating TA, Nichols WW, Vila J.

Antimicrob Agents Chemother. 2015;59(6):3059-65. doi: 10.1128/AAC.05136-14. Epub 2015 Mar 9.

13.

Antibacterial inhibitors of Gram-positive thymidylate kinase: structure-activity relationships and chiral preference of a new hydrophobic binding region.

Kawatkar SP, Keating TA, Olivier NB, Breen JN, Green OM, Guler SY, Hentemann MF, Loch JT, McKenzie AR, Newman JV, Otterson LG, Martínez-Botella G.

J Med Chem. 2014 Jun 12;57(11):4584-97. doi: 10.1021/jm500463c. Epub 2014 Jun 3.

PMID:
24828090
14.

New antibacterial agents: patent applications published in 2011.

Keating TA, Lister T, Verheijen JC.

Pharm Pat Anal. 2014 Jan;3(1):87-112. doi: 10.4155/ppa.13.65. Review.

PMID:
24354981
15.
16.

Sulfonylpiperidines as novel, antibacterial inhibitors of Gram-positive thymidylate kinase (TMK).

Martínez-Botella G, Loch JT, Green OM, Kawatkar SP, Olivier NB, Boriack-Sjodin PA, Keating TA.

Bioorg Med Chem Lett. 2013 Jan 1;23(1):169-73. doi: 10.1016/j.bmcl.2012.10.128. Epub 2012 Nov 5.

PMID:
23206863
17.

Discovery of selective and potent inhibitors of gram-positive bacterial thymidylate kinase (TMK).

Martínez-Botella G, Breen JN, Duffy JE, Dumas J, Geng B, Gowers IK, Green OM, Guler S, Hentemann MF, Hernandez-Juan FA, Joseph-McCarthy D, Kawatkar S, Larsen NA, Lazari O, Loch JT, Macritchie JA, McKenzie AR, Newman JV, Olivier NB, Otterson LG, Owens AP, Read J, Sheppard DW, Keating TA.

J Med Chem. 2012 Nov 26;55(22):10010-21. doi: 10.1021/jm3011806. Epub 2012 Oct 24.

PMID:
23043329
18.

In vivo validation of thymidylate kinase (TMK) with a rationally designed, selective antibacterial compound.

Keating TA, Newman JV, Olivier NB, Otterson LG, Andrews B, Boriack-Sjodin PA, Breen JN, Doig P, Dumas J, Gangl E, Green OM, Guler SY, Hentemann MF, Joseph-McCarthy D, Kawatkar S, Kutschke A, Loch JT, McKenzie AR, Pradeepan S, Prasad S, Martínez-Botella G.

ACS Chem Biol. 2012 Nov 16;7(11):1866-72. doi: 10.1021/cb300316n. Epub 2012 Aug 28.

PMID:
22908966
19.

In vitro validation of acetyltransferase activity of GlmU as an antibacterial target in Haemophilus influenzae.

Buurman ET, Andrews B, Gao N, Hu J, Keating TA, Lahiri S, Otterbein LR, Patten AD, Stokes SS, Shapiro AB.

J Biol Chem. 2011 Nov 25;286(47):40734-42. doi: 10.1074/jbc.M111.274068. Epub 2011 Oct 7.

20.

Correction for interference by test samples in high-throughput assays.

Shapiro AB, Walkup GK, Keating TA.

J Biomol Screen. 2009 Sep;14(8):1008-16. doi: 10.1177/1087057109341768. Epub 2009 Jul 30.

PMID:
19643982
21.

Exploitation of structural and regulatory diversity in glutamate racemases.

Lundqvist T, Fisher SL, Kern G, Folmer RH, Xue Y, Newton DT, Keating TA, Alm RA, de Jonge BL.

Nature. 2007 Jun 14;447(7146):817-22.

PMID:
17568739
22.

The structure of VibH represents nonribosomal peptide synthetase condensation, cyclization and epimerization domains.

Keating TA, Marshall CG, Walsh CT, Keating AE.

Nat Struct Biol. 2002 Jul;9(7):522-6.

PMID:
12055621
23.
24.

Chain termination steps in nonribosomal peptide synthetase assembly lines: directed acyl-S-enzyme breakdown in antibiotic and siderophore biosynthesis.

Keating TA, Ehmann DE, Kohli RM, Marshall CG, Trauger JW, Walsh CT.

Chembiochem. 2001 Feb 2;2(2):99-107. No abstract available.

PMID:
11828432
25.

The Ugi Five-Component Condensation Using CO(2), CS(2), and COS as Oxidized Carbon Sources.

Keating TA, Armstrong RW.

J Org Chem. 1998 Feb 6;63(3):867-871. No abstract available.

PMID:
11672085
26.

Tailoring enzymes that modify nonribosomal peptides during and after chain elongation on NRPS assembly lines.

Walsh CT, Chen H, Keating TA, Hubbard BK, Losey HC, Luo L, Marshall CG, Miller DA, Patel HM.

Curr Opin Chem Biol. 2001 Oct;5(5):525-34. Review.

PMID:
11578925
27.

Heterocycle formation in vibriobactin biosynthesis: alternative substrate utilization and identification of a condensed intermediate.

Marshall CG, Burkart MD, Keating TA, Walsh CT.

Biochemistry. 2001 Sep 4;40(35):10655-63.

PMID:
11524010
28.

Reconstitution and characterization of the Vibrio cholerae vibriobactin synthetase from VibB, VibE, VibF, and VibH.

Keating TA, Marshall CG, Walsh CT.

Biochemistry. 2000 Dec 19;39(50):15522-30.

PMID:
11112538
29.
30.
31.
33.

Initiation, elongation, and termination strategies in polyketide and polypeptide antibiotic biosynthesis.

Keating TA, Walsh CT.

Curr Opin Chem Biol. 1999 Oct;3(5):598-606. Review.

PMID:
10508662
35.

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